Search Results - "Gardell, S J"

Photoactivated γ-secretase inhibitors directed to the active site covalently label presenilin 1 by Gardell, Stephen J, Li, Yue-Ming, Xu, Min, Lai, Ming-Tain, Huang, Qian, Castro, José L, DiMuzio-Mower, Jillian, Harrison, Timothy, Lellis, Colin, Nadin, Alan, Neduvelil, Joseph G, Register, R. Bruce, Sardana, Mohinder K, Shearman, Mark S, Smith, Adrian L, Shi, Xiao-Ping, Yin, Kuo-Chang, Shafer, Jules A

“…Cleavage of amyloid precursor protein (APP) by the β- and γ-secretases generates the amino and carboxy termini, respectively, of the Aβ amyloidogenic peptides…”
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Effect of tiplaxtinin (PAI‐039), an orally bioavailable PAI‐1 antagonist, in a rat model of thrombosis by HENNAN, J. K., MORGAN, G. A., SWILLO, R. E., ANTRILLI, T. M., MUGFORD, C., VLASUK, G. P., GARDELL, S. J., CRANDALL, D. L.

“…Objective: To assess the antithrombotic and profibrinolytic effects of tiplaxtinin (PAI‐039), an orally bioavailable antagonist of PAI‐1, in rat models of…”
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Isolation, characterization, and cDNA cloning of a vampire bat salivary plasminogen activator by Gardell, S J, Duong, L T, Diehl, R E, York, J D, Hare, T R, Register, R B, Jacobs, J W, Dixon, R A, Friedman, P A

“…Vampire bat saliva contains a plasminogen activator that presumably assists these hematophagous animals during feeding. Here, we report that the vampire bat…”
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Potent Noncovalent Thrombin Inhibitors That Utilize the Unique Amino Acid d-Dicyclohexylalanine in the P3 Position. Implications on Oral Bioavailability and Antithrombotic Efficacy by Tucker, Thomas J, Lumma, William C, Lewis, S. Dale, Gardell, Stephen J, Lucas, Bobby J, Baskin, Elizabeth P, Woltmann, Richard, Lynch, Joseph J, Lyle, Elizabeth A, Appleby, Sandra D, Chen, I-Wu, Dancheck, Kimberley B, Vacca, Joseph P

“…In an effort to prepare orally bioavailable analogs of our previously reported thrombin inhibitor 1, we have synthesized a series of compounds that utilize the…”
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L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor by Sanderson, Philip E.J., Cutrona, Kellie J., Dorsey, Bruce D., Dyer, Dona L., McDonough, Colleen M., Naylor-Olsen, Adel M., Chen, I-Wu, Chen, Zhongguo, Cook, Jacquelynn J., Gardell, Stephen J., Krueger, Julie A., Lewis, S.Dale, Lin, Jiunn H., Lucas, Bobby J., Lyle, Elizabeth A., Lynch, Joseph J., Stranieri, Maria T., Vastag, Kari, Shafer, Jules A., Vacca, Joseph P.

“…Replacement of the amidinopiperidine P1 group of 3-benzylsulfonylamino-6-methyl-2-pyridinone acetamide thrombin inhibitor L-373,890 ( 2) with a mildly basic…”
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Presenilin 1 Is Linked with γ -Secretase Activity in the Detergent Solubilized State by Li, Yue-Ming, Lai, Ming-Tain, Xu, Min, Huang, Qian, DiMuzio-Mower, Jillian, Sardana, Mohinder K., Shi, Xiao-Ping, Yin, Kuo-Chang, Shafer, Jules A., Gardell, Stephen J.

“…γ -Secretase is a membrane-associated protease that cleaves within the transmembrane region of amyloid precursor protein to generate the C termini of the two…”
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Effect of the small molecule plasminogen activator inhibitor‐1 (PAI‐1) inhibitor, PAI‐749, in clinical models of fibrinolysis by LUCKING, A. J., VISVANATHAN, A., PHILIPPOU, H., FRASER, S., GRANT, P. J., CONNOLLY, T. M., GARDELL, S. J., FEUERSTEIN, G. Z., FOX, K. A. A., BOOTH, N. A., NEWBY, D. E.

“…Background: The principal inhibitor of fibrinolysis in vivo is plasminogen activator inhibitor‐1 (PAI‐1). PAI‐749 is a small molecule inhibitor of PAI‐1 with…”
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A novel rat carboxypeptidase, CPA2: characterization, molecular cloning, and evolutionary implications on substrate specificity in the carboxypeptidase gene family by Gardell, S J, Craik, C S, Clauser, E, Goldsmith, E J, Stewart, C B, Graf, M, Rutter, W J

“…A new member of the carboxypeptidase gene family, carboxypeptidase A2 (CPA2), has been identified from the predicted amino acid sequence of a rat pancreatic…”
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Vampire bat salivary plasminogen activator exhibits a strict and fastidious requirement for polymeric fibrin as its cofactor, unlike human tissue-type plasminogen activator. A kinetic analysis by BERGUM, P. W, GARDELL, S. J

“…The vampire bat salivary plasminogen activator (BatPA) is virtually inactive toward Glu-plasminogen in the absence of a fibrin-like cofactor, unlike human…”
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Structural characterization of the rat carboxypeptidase A1 and B genes. Comparative analysis of the rat carboxypeptidase gene family by Clauser, E, Gardell, S J, Craik, C S, MacDonald, R J, Rutter, W J

“…Nucleotide sequencing of a rat carboxypeptidase B (CPB) cDNA and direct sequencing of the CPB mRNA via primer extension on pancreatic polyadenylated RNA has…”
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Presenilin-1 and presenilin-2 exhibit distinct yet overlapping gamma-secretase activities by Lai, Ming-Tain, Chen, Elizabeth, Crouthamel, Ming-Chih, DiMuzio-Mower, Jillian, Xu, Min, Huang, Qian, Price, Eric, Register, R Bruce, Shi, Xiao-Ping, Donoviel, Dorit B, Bernstein, Alan, Hazuda, Daria, Gardell, Stephen J, Li, Yue-Ming

“…Presenilin-1 (PS1) and presenilin 2 (PS2) are proposed to be transmembrane aspartyl proteases that cleave amyloid precursor protein and Notch. PS1- and…”
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Assessment of thrombin inhibitor efficacy in a novel rabbit model of simultaneous arterial and venous thrombosis by Marsh Lyle, E, Lewis, S D, Lehman, E D, Gardell, S J, Motzel, S L, Lynch, Jr, J J

“…The importance of thrombin in arterial and venous thrombosis renders thrombin inhibition an important therapeutic target. Identification of novel inhibitors…”
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The search for the ideal thrombolytic agent: maximize the benefit and minimize the risk by Gardell, S J

“…Streptokinase, acylated plasminogen streptokinase complex, and tissue-type plasminogen activator (tPA) are widely used for the treatment of acute myocardial…”
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Discovery of a Novel, Selective, and Orally Bioavailable Class of Thrombin Inhibitors Incorporating Aminopyridyl Moieties at the P1 Position by Feng, Dong-Mei, Gardell, Stephen J, Lewis, S. Dale, Bock, Mark G, Chen, Zhongguo, Freidinger, Roger M, Naylor-Olsen, Adel M, Ramjit, Harri G, Woltmann, Richard, Baskin, Elizabeth P, Lynch, Joseph J, Lucas, Robert, Shafer, Jules A, Dancheck, Kimberley B, Chen, I-Wu, Mao, Shi-Shan, Krueger, Julie A, Hare, Timothy R, Mulichak, Anne M, Vacca, Joseph P

“…A novel class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position has been discovered. Four of these thrombin inhibitors (13b,c,e and…”
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Comparison of the bleeding potential of vampire bat salivary plasminogen activator versus tissue plasminogen activator in an experimental rabbit model by MONTONEY, M, GARDELL, S. J, MARDER, V. J

“…Vampire bat salivary plasminogen activator (Bat-PA) has significantly greater fibrin specificity than any of the fibrinolytic agents currently in clinical use…”
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C6 Modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption by Isaacs, Richard C.A., Cutrona, Kellie J., Newton, Christina L., Sanderson, Philip E.J., Solinsky, Mark G., Baskin, Elizabeth P., Chen, I-Wu, Cooper, Carolyn M., Cook, Jacquelynn J., Gardell, Stephen J., Lewis, S.Dale, Lucas, Robert J., Lyle, Elizabeth A., Lynch, Joseph J., Naylor-Olsen, Adel M., Stranieri, Maria T., Vastag, Kari, Vacca, Joseph P.

“…1 (L-374,087) is a potent, selective, efficacious, and orally bioavailable thrombin inhibitor that contains a core 3-amino-2-pyridinone moiety. Replacement of…”
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Combinatorial mutagenesis of the reactive site region in plasminogen activator inhibitor I by York, J D, Li, P, Gardell, S J

“…Plasminogen activator inhibitor (PAI-I) rapidly inactivates tissue plasminogen activator (t-PA) and urokinase (UK) with nearly identical association rate…”
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Vampire bat salivary plasminogen activator promotes robust lysis of plasma clots in a plasma milieu without causing fluid phase plasminogen activation by Hare, T R, Gardell, S J

“…Vampire bat salivary plasminogen activator (BatPA), human tissue-type plasminogen activator (tPA) or streptokinase (SK) were incubated in human citrated plasma…”
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Effective thrombolysis without marked plasminemia after bolus intravenous administration of vampire bat salivary plasminogen activator in rabbits by GARDELL, S. J, RAMJIT, D. R, SHEBUSKI, R. J, STABILITO, I. I, FUJITA, T, LYNCH, J. J, CUCA, G. C, JAIN, D, WANG, S, JWU-SHENG TUNG, MARK, G. E

“…The use of recombinant tissue-type plasminogen activator (t-PA) in thrombolytic therapy is frequently associated with significant fibrinogenolysis. In…”
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Vampire bat salivary plasminogen activator evokes minimal bleeding relative to tissue-type plasminogen activator as assessed by a rabbit cuticle bleeding time model by Mellott, M J, Ramjit, D R, Stabilito, I I, Hare, T R, Senderak, E T, Lynch, Jr, J J, Gardell, S J

“…Cuticle bleeding time (CBT) measurements in anesthetized rabbits were performed to assess the potential bleeding risks which may accompany the administration…”
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